Synthesis and biological activity of 5-substituted anti-constrained acyclic analogs of cytidine and uridine

被引：7

作者：

Hsu, LY ^{[1
]}

Chang, YM ^{[1
]}

Lin, CH ^{[1
]}

Drach, JC ^{[1
]}

机构：

[1] UNIV MICHIGAN,SCH DENT,DEPT BIOL & MAT SCI,ANN ARBOR,MI 48109

来源：

NUCLEOSIDES & NUCLEOTIDES | 1996年 / 15卷 / 11-12期

关键词：

D O I：

10.1080/07328319608002736

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A number of 5-substituted constrained acyclic analogs of cytidine and uridine have been prepared in which the glycosyl torsion angle is constrained in the anti conformation. Compounds 2a-c, 3a-c, 4, 5 and 6 were tested for activity against HCMV and HSV-1. Compounds 2a and 2b showed moderate activity against HCMV. Compound 2c exhibited a weak inhibitory activity against HSV-1. Compounds 2a, 3a,4, 5, 6, 8, and 9 were screened for their anti-HIV or antitumor activity. None of them were active against HIV. However, compound 9 showed a 50% inhibition on MDA-MB-231/ATTC breast cancer cell growth at a concentration of 0.15 mu M.

引用

页码：1835 / 1847

页数：13

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